Selective Inhibitors/Activators of PDE3 for Treatment of Heart Failure and Vascular Disease

Nonselective cyclic nucleotide phosphodiesterase (PDE3) hydrolyzes cAMP and regulate its content in cardiac myocytes. PDE3 inhibitors are already used clinically in the treatment of heart failure and peripheral vascular disease. The increased morbidity and mortality seen with the long-term administration of these agents in patients with heart failure severely limits the benefits that can be achieved through their use. Dr. Movsesian has identified new PDE3 isoforms in human myocardium that are localized to different interacellular compartments of cardiac myocytes, which are regulated by different mechanisms. He has also developed methods to identify selective activators and inhibitors of these isoforms. The novel activators or inhibitors could be used in the treatment of a variety of cardiac and vascular disease.

We anticipate applicability to the treatment of heart failure, systemic and pulmonary hypertension, cardiac transplantation, coronary artery disease (particularly post-angioplasty), peripheral vascular disease, diabetes and hypercoagulabe states, including venous thromboembolism

Stage of Development
A formal US patent application (20030158133A1) has been filed with the USPTO and pending. European patent application (WO03012030) and a Japan application have been filed and pending.
This technology is part of an active and ongoing research program and is seeking partners for development of the working product. It is available for developmental research support and licensing under either exclusive or non-exclusive terms.

Additional Info
*Hambleton R, Krall J, Tikishvili E, Honeggar M, Ahmad F, Manganiello VC, Movsesian MA. (2005) Isoforms of cyclic nucleotide phosphodiesterase PDE3 and their contribution to cAMP hydrolytic activity in subcellular fractions of human myocardium.J Biol Chem. 280(47):39168-74.

Inventor(s): Matthew Movsesian

Type of Offer: Licensing

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